New method for synthesizing dasatinib

A technology of dasatinib and a new method, which is applied in the field of synthesizing dasatinib, can solve the problems of high production cost, harsh reaction conditions, and unfriendly environment, and achieve the effects of low production cost, mild reaction conditions, and environmental friendliness
CN102010407AInactive Publication Date: 2011-04-13SHANGHAI SYNCORES TECH INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI SYNCORES TECH INC
Publication Date
2011-04-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a new method for synthesizing dasatinib. The method comprises the following steps: a compound 38 and a compound 8 are subjected to amidation reaction to obtain a compound 7; and the compound 7 reacts with a compound 10 under alkaline condition to obtain dasatinib I. The method provided by the invention has the following advantages: the method is mild in reaction conditions, simple to operate, convenient for purification, low in production cost, environmental-friendly and suitable for industrial production.
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Description

technical field

[0001] The invention relates to medicinal chemistry, in particular to a new method for synthesizing dasatinib. Background technique

[0002] Dasatinib, the chemical name is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]- 2-methyl-4-pyrimidinyl] amino]-5-thiazole carboxamide, its structural formula is as follows:

[0003]

[0004] Dasatinib is a polytyrosine kinase inhibitor, which is the first oral chemotherapy drug capable of inhibiting multiple configurations of tyrosine protein kinase Abl. At nanomolar concentrations, the drug inhibits multiple kinases of the BCR-ABL kinase family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFR-B. By inhibiting the above-mentioned kinases, dasatinib can inhibit the proliferation of leukemia cells in the bone marrow of CML and Ph+ ALL, but normal red blood cells, white blood cells and platelets can still continue to proliferate.

[0005] The synthetic route of existing dasatinib (I) mainly contains...

Claims

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